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3-Deazaneplanocin A

Cat. No. M2358
3-Deazaneplanocin A  Structure
Synonym:

NSC 617989; 3-Deazaneplanocin; DZNep

Size Price Availability
1mg USD 100  USD100 Out of stock
5mg USD 440  USD440 Out of stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

3-Deazaneplanocin-A, a carbocyclic analog of adenosine, was synthesized as an inhibitor of -adenosylhomocysteine hydrolase. 3-Deazaneplanocin-A treatment induced apoptosis in cultured and primary AML cells. In addition, 3-Deazaneplanocin A depletes EZH2 levels, and inhibits trimethylation of lysine 27 on histone H3 in the HL-60 and OCI-AML3 cells and in primary AML cells. 3-Deazaneplanocin A treatment induces p16, p21, p27, and FBXO32 while depleting cyclin E and HOXA9 levels.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 262.26
Formula C12H14N4O3
CAS Number 102052-95-9
Purity >98%
Solubility DMSO 40 mg/mL
Storage at -20°C
References

[1] Fiskus W, et al. Blood. Combined epigenetic therapy with the histone methyltransferase EZH2 inhibitor 3-deazaneplanocin A and the histone deacetylase inhibitor panobinostat against human AML cells.

[2] Glazer RI, et al. Biochem Pharmacol. 3-Deazaneplanocin A: a new inhibitor of S-adenosylhomocysteine synthesis and its effects in human colon carcinoma cells.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: 3-Deazaneplanocin A , NSC 617989; 3-Deazaneplanocin; DZNep supplier, Histone Methyltransferase, inhibitors

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